This invention relates to certain 10,11-furo; and 10,11-bis-(hydroxyalkyl)-cyproheptadine derivatives (structures I - II, and III, respectively, below) having anticholinergic, but little to no antiserotonin or antihistamine activity. This invention also relates to processes for the preparation of such derivative compounds, pharmaceutical compositions comprising such compounds; and methods of treatment comprising administering such compounds and compositions. ##STR1##
With respect to the above structures which represent the compounds of the present invention, R.sub.2 is lower alkyl having from 1 to about 5 carbon atoms; and R.sub.1 is hydrogen, or lower alkyl having from 1 to about 5 carbon atoms.
The parent compound, cyproheptadine, is a known pharmaceutical having potent antihistamine, antiserotonin and anticholinergic activity. Unexpectedly, however, the compounds of this invention are exclusively anticholinergics with little or no antihistamine and antiserotonic activity.
Thus, it is an object of the present invention to prepare cyproheptadine derivatives which specifically act as anticholinergics and are free of ancillary pharmacological effects such as those associated with the parent compound, namely: antihistamine and antiserotonin activity.
It is a further object of the present invention to provide processes for the preparation of such cyproheptadine derivative compounds; to provide pharmaceutical compositions comprising such compounds; and to provide methods of treatment comprising administering such compounds and compositions, wherein anticholinergic activity is desired and wherein antihistamine/ antiserotonin effects are not indicated.